Medically reviewed on August 12, 2018
(al oh GLIP tin)
- Alogliptin Benzoate
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Nesina: 6.25 mg, 12.5 mg, 25 mg
Generic: 6.25 mg, 12.5 mg, 25 mg
Brand Names: U.S.
- Antidiabetic Agent, Dipeptidyl Peptidase 4 (DPP-4) Inhibitor
Alogliptin inhibits dipeptidyl peptidase 4 (DPP-4) enzyme resulting in prolonged active incretin levels. Incretin hormones (eg, glucagon-like peptide-1 [GLP-1] and glucose-dependent insulinotropic polypeptide [GIP]) regulate glucose homeostasis by increasing insulin synthesis and release from pancreatic beta cells and decreasing glucagon secretion from pancreatic alpha cells. Decreased glucagon secretion results in decreased hepatic glucose production. Under normal physiologic circumstances, incretin hormones are released by the intestine throughout the day and levels are increased in response to a meal; incretin hormones are rapidly inactivated by the DPP-4 enzyme.
Extensive (~100%) regardless of food intake
Not extensively metabolized; minor metabolism via CYP2D6 and CYP3A4 suggested by in vitro studies (<7% of parent compound is transformed to active and inactive metabolites)
Urine 76% (60% to 71% as unchanged drug); feces 13%
Time to Peak
~1 to 2 hours
Special Populations: Renal Function Impairment
AUC increased two-, three-, and four-fold in patients with moderate renal impairment, severe renal impairment, and end-stage renal disease, respectively.
Use: Labeled Indications
Diabetes mellitus, type 2: Management of adults with type 2 diabetes mellitus (noninsulin dependent, NIDDM) as an adjunct to diet and exercise as monotherapy or in combination therapy
History of serious hypersensitivity (eg, anaphylaxis, angioedema, severe cutaneous reactions) to alogliptin or any component of the formulation
Diabetes mellitus, type 2: Oral: 25 mg once daily
Concomitant use with insulin and/or insulin secretagogues (eg, sulfonylureas): Reduced dose of insulin and/or insulin secretagogues may be needed.
Refer to adult dosing.
Dosing: Renal Impairment
CrCl ≥60 mL/minute: No dosage adjustment necessary.
CrCl ≥30 to <60 mL/minute: 12.5 mg once daily
CrCl ≥15 to <30 mL/minute: 6.25 mg once daily
ESRD (CrCl <15 mL/minute or requiring hemodialysis): 6.25 mg once daily; administered without regard to timing of hemodialysis
Peritoneal dialysis: There is no dosage adjustment provided in the manufacturer’s labeling (has not been studied).
Dosing: Hepatic Impairment
Mild or moderate impairment (Child-Pugh class A or B): No dosage adjustment necessary. Use with caution.
Severe impairment (Child-Pugh class C): There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).
Persistent or worsening clinically significant liver enzyme elevations during treatment: Interrupt treatment and investigate probable cause; do not reinitiate if explanation for the liver test abnormalities cannot be determined.
May be taken with or without food.
Individualized medical nutrition therapy (MNT) based on ADA recommendations is an integral part of therapy.
Store at 25°C (77°F); excursions permitted between 15°C to 30°C (59°F to 86°F).
Alpha-Lipoic Acid: May enhance the hypoglycemic effect of Antidiabetic Agents. Monitor therapy
Androgens: May enhance the hypoglycemic effect of Blood Glucose Lowering Agents. Exceptions: Danazol. Monitor therapy
Angiotensin-Converting Enzyme Inhibitors: Dipeptidyl Peptidase-IV Inhibitors may enhance the adverse/toxic effect of Angiotensin-Converting Enzyme Inhibitors. Specifically, the risk of angioedema may be increased. Monitor therapy
Guanethidine: May enhance the hypoglycemic effect of Antidiabetic Agents. Monitor therapy
Hyperglycemia-Associated Agents: May diminish the therapeutic effect of Antidiabetic Agents. Monitor therapy
Hypoglycemia-Associated Agents: Antidiabetic Agents may enhance the hypoglycemic effect of Hypoglycemia-Associated Agents. Monitor therapy
Insulins: Dipeptidyl Peptidase-IV Inhibitors may enhance the hypoglycemic effect of Insulins. Management: Consider a decrease in insulin dose when initiating therapy with a dipeptidyl peptidase-IV inhibitor and monitor patients for hypoglycemia. Consider therapy modification
Monoamine Oxidase Inhibitors: May enhance the hypoglycemic effect of Blood Glucose Lowering Agents. Monitor therapy
Pegvisomant: May enhance the hypoglycemic effect of Blood Glucose Lowering Agents. Monitor therapy
Prothionamide: May enhance the hypoglycemic effect of Blood Glucose Lowering Agents. Monitor therapy
Quinolones: May enhance the hypoglycemic effect of Blood Glucose Lowering Agents. Quinolones may diminish the therapeutic effect of Blood Glucose Lowering Agents. Specifically, if an agent is being used to treat diabetes, loss of blood sugar control may occur with quinolone use. Monitor therapy
Ritodrine: May diminish the therapeutic effect of Antidiabetic Agents. Monitor therapy
Salicylates: May enhance the hypoglycemic effect of Blood Glucose Lowering Agents. Monitor therapy
Selective Serotonin Reuptake Inhibitors: May enhance the hypoglycemic effect of Blood Glucose Lowering Agents. Monitor therapy
Sulfonylureas: Dipeptidyl Peptidase-IV Inhibitors may enhance the hypoglycemic effect of Sulfonylureas. Management: Consider a decrease in sulfonylurea dose when initiating therapy with a dipeptidyl peptidase-IV inhibitor and monitor patients for hypoglycemia. Consider therapy modification
Thiazide and Thiazide-Like Diuretics: May diminish the therapeutic effect of Antidiabetic Agents. Monitor therapy
1% to 10%:
Cardiovascular: Cardiac failure (4%)
Central nervous system: Headache (4%)
Genitourinary: Decreased estimated GFR (5%)
Hepatic: Increased serum ALT (>3 times ULN: 1%)
Renal: Renal function abnormality (3%; patients with high cardiovascular risk: 23%), renal disease (patients with high cardiovascular risk: 17%), renal insufficiency (patients with high cardiovascular risk: 8%)
Respiratory: Nasopharyngitis (5%), upper respiratory tract infection (5%)
<1%, postmarketing, and/or case reports: Anaphylaxis, angioedema, constipation, decreased creatinine clearance, diarrhea, hepatic failure, hypersensitivity reaction, increased liver enzymes, intestinal obstruction, nausea, pancreatitis, serum sickness, severe arthralgia (FDA Safety Alert, Aug 28, 2015), skin rash, Stevens-Johnson syndrome, urticaria
Concerns related to adverse effects:
• Arthralgia: Severe and disabling arthralgia has been reported with DPP-4 inhibitor use; onset may occur within one day to years after treatment initiation and may resolve with discontinuation of therapy. Some patients may experience a recurrence of symptoms if DPP-4 inhibitor therapy resumed. Discontinue use if severe joint pain results from DPP-4 inhibitor therapy.
• Bullous pemphigoid: DPP-4 inhibitor use has been associated with development of bullous pemphigoid; cases have typically resolved with topical or systemic immunosuppressive therapy and discontinuation of DPP-4 inhibitor therapy. Advise patients to report development of blisters or erosions. Discontinue therapy if bullous pemphigoid is suspected and consider referral to a dermatologist.
• Hepatotoxicity: Cases of fatal and nonfatal hepatic failure have been reported in postmarketing surveillance. Baseline liver function tests (serum transaminases) are recommended to rule out underlying liver diseases. Use with caution in patients with abnormal serum transaminases. Monitor and promptly evaluate serum transaminase levels in patients with symptoms of hepatic injury (eg, fatigue, anorexia, jaundice, dark urine, and/or abdominal pain). In patients with clinically significant transaminase elevations and/or persistent or worsening elevations, alogliptin therapy should be interrupted. Therapy should only be resumed with caution in patients where an alternative cause of transaminase elevations has been determined.
• Hypersensitivity reactions: Rare hypersensitivity reactions, including anaphylaxis, angioedema, and/or severe dermatologic reactions such as Stevens-Johnson syndrome, have been reported in postmarketing surveillance; discontinue if signs/symptoms of hypersensitivity reactions occur. Use with caution if patient has experienced angioedema with other DPP-4 inhibitor use.
• Pancreatitis: Cases of acute pancreatitis have been reported with use. Monitor for signs/symptoms of pancreatitis; discontinue use immediately if pancreatitis is suspected and initiate appropriate management. Use with caution in patients with a history of pancreatitis as it is not known if this population is at greater risk.
• Heart failure: In a multi-center, randomized, double-blind, placebo-controlled cardiovascular outcome trial of patients with type 2 diabetes and recent acute coronary syndrome, treatment with alogliptin was not associated with increased risk of hospitalization for heart failure (Zannad 2015). The manufacturer recommends using alogliptin with caution in patients with a history of heart failure and renal impairment. Monitor for signs and symptoms of heart failure during therapy and consider discontinuation of therapy if heart failure develops.
• Hepatic impairment: Use with caution in patients with hepatic dysfunction.
• Renal impairment: Use with caution in patients with moderate-to-severe renal dysfunction and end-stage renal disease (ESRD) requiring hemodialysis; dosing adjustment required.
Concurrent drug therapy issues:
• Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.
• Appropriate use: Not indicated for use in patients with type 1 diabetes mellitus (insulin dependent, IDDM) or with diabetic ketoacidosis (DKA).
• Patient education: Diabetes self-management education (DSME) is essential to maximize the effectiveness of therapy.
HbA1c (at least twice yearly in patients who have stable glycemic control and are meeting treatment goals; quarterly in patients not meeting treatment goals or with therapy change [ADA 2018a]), serum glucose; renal function prior to initiation and periodically during treatment; baseline liver function tests and then as clinically indicated; signs/symptoms of pancreatitis; signs/symptoms of heart failure
Adverse events were not observed in animal reproduction studies.
In women with diabetes, maternal hyperglycemia can be associated with congenital malformations as well as adverse effects in the fetus, neonate, and the mother (ACOG 2005; ADA 2018c; Metzger 2007). To prevent adverse outcomes prior to conception and throughout pregnancy, maternal blood glucose and HbA1c should be kept as close to target goals as possible but without causing significant hypoglycemia (ADA 2018c; Blumer 2013). Agents other than alogliptin are currently recommended to treat diabetes in pregnant women (ADA 2018c).
• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)
• Patient may experience signs of common cold, pharyngitis, rhinitis, rhinorrhea, or headache. Have patient report immediately to prescriber severe joint pain, persistent joint pain, skin blisters, skin breakdown, signs of heart problems (cough or shortness of breath that is new or worse, swelling of the ankles or legs, abnormal heartbeat, weight gain of more than five pounds in 24 hours, dizziness, or passing out), signs of low blood sugar (dizziness, headache, fatigue, feeling weak, shaking, a fast heartbeat, confusion, hunger, or sweating), signs of pancreatitis (severe abdominal pain, severe back pain, severe nausea, or vomiting), signs of liver problems (dark urine, fatigue, lack of appetite, nausea, abdominal pain, light-colored stools, vomiting, or jaundice), or signs of Stevens-Johnson syndrome/toxic epidermal necrolysis (red, swollen, blistered, or peeling skin [with or without fever]; red or irritated eyes; or sores in mouth, throat, nose, or eyes) (HCAHPS).
• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.
Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.
More about alogliptin
- Alogliptin Side Effects
- During Pregnancy
- Dosage Information
- Drug Interactions
- Support Group
- En Español
- 4 Reviews
- Drug class: dipeptidyl peptidase 4 inhibitors
Other brands: Nesina